通过有机催化剂介导的,经济的拉塔诺普罗斯特的总合成
Genki Kawauchi1, Yurina Suga1, Shunsuke Toda1
1Department of Chemistry, Graduate School of Science, Tohoku University Sendai 980-8578 Japan yujiro.hayashi.b7@tohoku.ac.jp.
Chemical science
|September 29, 2023
概括
这项研究提出了一种新的,高效的合成latanoprost,一个关键的抗葡萄糖瘤药物. 六种的酶选择性全合成实现了高纯度和产量,为这种重要的药物提供了一条实用的途径.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
背景情况:
- 拉坦诺普罗斯特是治疗青光眼的关键药物.
- 复杂药物剂的高效和对抗选择性合成至关重要.
研究的目的:
- 为了开发一个经济和enantioselective的拉坦诺普罗斯特的总合成.
- 在合成中实现高的二聚体选择性和选择性.
主要方法:
- 一种六个容器的合成,采用关键反应:克里什合,烯基转化,有机催化迈克尔反应,Mukaiyama aldol反应和乙烯基酸盐添加.
- 利用基质控制反应和催化方法提高效率.
主要成果:
- 在整个合成过程中实现了出色的二聚体选择性和酶选择性.
- 成功合成了近乎光学纯净的拉坦诺普罗斯特,总产量为24%,以经济的方式.
结论:
- 开发的合成途径是高效和高度选择性的.
- 这种方法为大规模生产拉坦诺普罗斯特提供了可行的途径.
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